4939-28-0Relevant articles and documents
The Ag-promoted α-C-H arylation of alcohols
Wang, Shoufeng,Xing, Shuya,Zhang, Yingying,Fan, Yafei,Zhao, Huaiqing,Wang, Jianfeng,Zhang, Shuxiang,Wang, Wengui
, p. 41847 - 41850 (2019)
We herein report the functionalization of α-C-H in alcohols through cross-dehydrogenative coupling reactions. Selectfluor was used as a mild oxidant. In situ-generated HF participated in the reaction and no external strong acid was necessary. A variety of heteroaryl-substituted alcohols were achieved with good yields and with good functional group tolerance.
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity
Li, Wenlong,Xu, Feijie,Shuai, Wen,Sun, Honghao,Yao, Hong,Ma, Cong,Xu, Shengtao,Yao, Hequan,Zhu, Zheying,Yang, Dong-Hua,Chen, Zhe-Sheng,Xu, Jinyi
, p. 993 - 1013 (2019/01/11)
A series of novel quinoline-chalcone derivatives were designed, synthesized, and evaluated for their antiproliferative activity. Among them, compound 24d exhibited the most potent activity with IC50 values ranging from 0.009 to 0.016 μM in a panel of cancer cell lines. Compound 24d also displayed a good safety profile with an LD50 value of 665.62 mg/kg by intravenous injection, and its hydrochloride salt 24d-HCl significantly inhibited tumor growth in H22 xenograft models without observable toxic effects, which was more potent than that of CA-4. Mechanism studies demonstrated that 24d bound to the colchicine site of tubulin, arrested the cell cycle at the G2/M phase, induced apoptosis, depolarized mitochondria, and induced reactive oxidative stress generation in K562 cells. Moreover, 24d has potent in vitro antimetastasis and in vitro and in vivo antivascular activities. Collectively, our findings suggest that 24d deserves to be further investigated as a potent and safe antitumor agent for cancer therapy.
Preparation method of 2-methyl-4-hydroxymethyl quinoline and derivatives thereof
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Paragraph 0015; 0017; 0029-0038, (2019/06/07)
The invention belongs to the technical field of chemical synthesis, and particularly relates to a method for reacting 2-methylquinoline and derivatives thereof with primary alcohol. The method is carried out by the following steps of: under the catalysis of Selectfluor/AgNO3, reacting the 2-methylquinoline and the derivatives in a primary alcohol aqueous solution, and performing column chromatography to obtain a product of dehydrogenation coupling of 4-position and alcohol compounds of the 2-methylquinoline derivatives. The method provided by the invention is carried out in a mixed solution ofwater and alcohol compounds under the catalysis of Selectfluor/AgNO3, and has the advantages of good substrate solubility, wide applicability, high reaction yield and strong controllability. The method is green and environment-friendly, and has the advantages of few side reaction products, green and high efficiency.